gedatolisib
Small moleculeexperimental
Gedatolisib (PF-05212384) is an experimental drug for treatment of cancer in development by Celcuity, Inc. The mechanism of action is accomplished by binding the different p110 catalytic subunit isoforms of PI3K and the kinase site of mTOR. — Wikipedia
Clinical trial activity
21 trials · 16 clinical orgs · 0 marketing orgs
Phase 1
14
Phase 2
11
Phase 3
2
Phase 4
0
Earliest trial started Jan 1, 2010 (NCT00940498)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Colorectal Neoplasms · Phase 2
- Endometrial Neoplasms · Phase 2
- Genital Diseases, Male · Phase 1/Phase 2
- Head and Neck Neoplasms · Phase 1
- Healthy Volunteers · Phase 1
- Leukemia, Myeloid, Acute · Phase 2
- Lung Neoplasms · Phase 1
- Male Urogenital Diseases · Phase 1/Phase 2
- Neoplasms · Phase 1
- Ovarian Neoplasms · Phase 1
- Pancreatic Neoplasms · Phase 1
- Prostatic Diseases · Phase 1/Phase 2
- Prostatic Neoplasms · Phase 1/Phase 2
- Prostatic Neoplasms, Castration-Resistant · Phase 1/Phase 2
- Small Cell Lung Carcinoma · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 1
- Triple Negative Breast Neoplasms · Phase 1
Mechanism of action
- Serine/threonine-protein kinase mTORINHIBITOR
MTOR inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 inhibitor
- PI3-kinase class IINHIBITOR
PI3-kinase class I inhibitor
Dual MTOR/PIK3 inhibitor, ATP-competitive mTORC1/mTORC2 inhibitor
- Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PIK3CG) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) ↗
- Phosphatidylinositol 3-kinase regulatory subunit beta (PIK3R2) ↗
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) ↗
- Phosphoinositide 3-kinase regulatory subunit 5 (PIK3R5) ↗
- Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) ↗
- PI3-kinase p85-alpha subunit
- PI3-kinase p110-delta subunit
- PI3-kinase p110-alpha subunit
- PI3-kinase p110-gamma subunit
- PI3-kinase p110-beta subunit
- PI3-kinase p85-beta subunit
- PI3-kinase p110-delta/p85-alpha
- PI3-kinase p110-alpha/p85-alpha
- PI3K p110 beta/p85 alpha
- PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5
- Phosphatidylinositol 3-kinase regulatory subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform
- PIK3CG/PIK3R1
- Phosphatidylinositol 3-kinase regulatory subunit gamma
Chemistry & pharmacology
Loading structure…
SMILES
CN(C)C1CCN(C(=O)c2ccc(NC(=O)Nc3ccc(-c4nc(N5CCOCC5)nc(N5CCOCC5)n4)cc3)cc2)CC1- Mol. weight
- 615.74 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaGedatolisib ↗
- ChEMBLCHEMBL592445 ↗
Also known as
- 1-(4-((4-(dimethylamino)piperidin-1-yl)carbonyl)phenyl)-3-(4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl)urea
- gedatolisib
- gedatolisib
- gedatolisib
- gedatolisib
- pf-05212384
- pf-05212384
- pf-05212384
- pf-05212384
- pki587
- pki 587
- pki-587
- pki-587
- pki-587
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06757634 | Phase 3 | Jun 30, 2025 | Celcuity |
| NCT06190899 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2024 | Celcuity |
| NCT05501886 | Phase 3 | Sep 30, 2022 | Celcuity |
| NCT03911973 | Phase 1/Phase 2 (Phase 2) | May 31, 2019 | Big Ten Cancer Research Consortium, Pfizer, University of Wisconsin |
| NCT03698383 | Phase 2 | Oct 31, 2018 | Seoul National University |
| NCT03400254 | Phase 1/Phase 2 (Phase 2) | Feb 28, 2018 | Translational Breast Cancer Research Consortium (TBCRC), University of Pennsylvania |
| NCT03243331 | Phase 1 | Jan 19, 2018 | Indiana University |
| NCT02920450 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2017 | Pfizer, University of Florida |
| NCT03065062 | Phase 1 | Feb 28, 2017 | Harvard University, Pfizer |
| NCT02684032 | Phase 1 | Jun 14, 2016 | Pfizer |
| NCT02626507 | Phase 1 | Jan 1, 2016 | Eastchester Center for Cancer Care |
| NCT02438761 | Phase 2 | Aug 31, 2015 | Curie Institute, Fondation ARC, National Cancer Institute, France |
| NCT02142920 | Phase 1 | Jul 1, 2014 | Pfizer |
| NCT02069158 | Phase 1 | Apr 1, 2014 | Oncology Institute of Southern Switzerland, Ospedale S. Giovanni Bellinzona |
| NCT01937715 | Phase 1/Phase 2 (Phase 2) | Feb 1, 2014 | Pfizer |
| NCT01925274 | Phase 2 | Nov 1, 2013 | Pfizer |
| NCT01920061 | Phase 1 | Sep 10, 2013 | Pfizer |
| NCT01420081 | Phase 2 | Jan 1, 2012 | Pfizer |
| NCT01347866 | Phase 1 | Oct 1, 2011 | Pfizer |
| NCT00940498 | Phase 1 | Jan 1, 2010 | Pfizer |
Showing 20 of 21 trials
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Organizations
Research & Development (16)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 11 | 8 | 2 | 2010 |
| Celcuity | For profit | 4 | 4 | 3 | 2022 |
| Big Ten Cancer Research Consortium | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Curie Institute | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Eastchester Center for Cancer Care | Academic/Hospital | 1 | 1 | 1 | 2016 |
| Fondation ARC | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Indiana University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| National Cancer Institute, France | Government | 1 | 0 | 1 | 2015 |
| Oncology Institute of Southern Switzerland | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Ospedale S. Giovanni Bellinzona | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Seoul National University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Translational Breast Cancer Research Consortium (TBCRC) | Academic/Hospital | 1 | 0 | 1 | 2018 |
| University of Florida | Academic/Hospital | 1 | 1 | 1 | 2017 |
| University of Pennsylvania | Academic/Hospital | 1 | 1 | 1 | 2018 |
| University of Wisconsin | Academic/Hospital | 1 | 1 | 1 | 2019 |
16 organizations
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